mGluR5 antagonist-1
Based on 1 Customer Validation
mGluR5 antagonist-1 is an orally active mGluR5 antagonist with an IC50 value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect. mGluR5 antagonist-1 can be used for the study of depressive disorder.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.80%
- No. CAS: 2761424-76-2
- Fòrmula: C23H18N4O2
- Peso molecular:382.41
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (2 months; 20-23 g) bearing chronic unpredictable mild stress (CUMS)[1]
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Dosage:5, 10, 20 mg/kg
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Administration:Oral gavage (i.g); once a day; for 3 consecutive days
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Result:The factors for identifying sensitivity to depression-like behaviors (including GluA1, GluA2, p-PKA, BDNF and TrkB) could be improved.
Chemical Information
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No. CAS 2761424-76-2
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Appearance Solid
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Peso molecular 382.41
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Fòrmula C23H18N4O2
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Color Light yellow to yellow
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SMILES
CN1C2=NC=NC(C#CC3=CC=CC=C3)=C2C=C1C(NC4=CC=C(OC)C=C4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 200 mg/mL (523.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.07 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6150 mL | 13.0750 mL | 26.1499 mL | 65.3749 mL |
| 5 mM | 0.5230 mL | 2.6150 mL | 5.2300 mL | 13.0750 mL | |
| 10 mM | 0.2615 mL | 1.3075 mL | 2.6150 mL | 6.5375 mL | |
| 15 mM | 0.1743 mL | 0.8717 mL | 1.7433 mL | 4.3583 mL | |
| 20 mM | 0.1307 mL | 0.6537 mL | 1.3075 mL | 3.2687 mL | |
| 25 mM | 0.1046 mL | 0.5230 mL | 1.0460 mL | 2.6150 mL | |
| 30 mM | 0.0872 mL | 0.4358 mL | 0.8717 mL | 2.1792 mL | |
| 40 mM | 0.0654 mL | 0.3269 mL | 0.6537 mL | 1.6344 mL | |
| 50 mM | 0.0523 mL | 0.2615 mL | 0.5230 mL | 1.3075 mL | |
| 60 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0896 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3269 mL | 0.8172 mL | |
| 100 mM | 0.0261 mL | 0.1307 mL | 0.2615 mL | 0.6537 mL |
mGluR5 antagonist-1 Related Classifications
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